β-Secretase inhibition by C-methylisoflavones from Abronia nana.

Yang, Eun-Ju; Lee, Taeho; Song, Kyung-Sik

The methanol extract of Abronia nana suspension cultures were subjected to column chromatography to identify potential inhibitors of β-secretase, which is a major factor in Alzheimer's disease development. Two new C-methylisoflavones boeravinone T (1) and U (4) were isolated with three knowns boeravinone B (2), J (3) and X (5). The half-maximal inhibitory concentration (IC50) values of compounds 1–5 were 18.29, 8.57, 7.87, 12.02 and 5.30 μM, respectively. The most potent 5, non-competitively inhibited β-secretase [inhibition constant (Ki) = 3.79 μM]. Compounds 1–5 did not inhibit other proteases such as chymotrypsin, trypsin and elastase at concentrations up to 1 mM, indicating that they were relatively specific inhibitors of β-secretase. A free hydroxyl group at C-3 position of the C-methylisoflavone skeleton appeared to be responsible for the stronger inhibitory activity against β-secretase.

SECRETASES; METHANOL; HERBAL medicine; COLUMN chromatography; ALZHEIMER'S disease

Natural Product Research, 2019, Vol 33, Issue 12, p1705

1478-6419

Academic Journal

10.1080/14786419.2018.1431637